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    • 82. 发明申请
    • 4,9-ETHANO-BENZO(F)ISOINDOLE DERIVATIVES AS FARNESYL TRANSFERASE INHIBITORS
    • 4,9-ETHANO-BENZO(F)作为FARNESYL转移酶抑制剂的ISO衍生物
    • WO1997003050A1
    • 1997-01-30
    • PCT/FR1996001062
    • 1996-07-08
    • RHONE-POULENC RORER S.A.COMMERÇON, AlainLEBRUN, AlainMAILLIET, PatrickPEYRONEL, Jean-FrançoisSOUNIGO, FabienneTRUCHON, AlainZUCCO, Martine
    • RHONE-POULENC RORER S.A.
    • C07D209/72
    • C07D209/72C07F9/5728
    • Novel products of general formula (I), preparation thereof and pharmaceutical compositions containing said products are disclosed. In general formula (I), R is a radical of general formula -(CH2)m-X1-(CH2)n-Z, where X1 is a simple bond or O or S, n is 0 or 1 and n is 0, 1 or 2, the CH2 radicals being optionally substituted by carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, amino, alkylamino or dialkylamino, and Z is carboxy, COOR4, where R4 is alkyl, or CON(R5)(R6), where R5 is hydrogen or alkyl and R6 is hydrogen or optionally substituted alkyl, or else R5 is hydrogen or alkyl and R6 is hydroxy, optionally substituted alkyloxy or amino, or PO(OR7)2, where R7 is hydrogen or alkyl; or a radical -NH-CO-T where T is hydrogen or optionally substituted alkyl; or else a radical (a); R1 and R2 are hydrogen or halogen or optionally substituted alkyloxy or alkyl, or else R1 and R2 in ortho positions form a heterocyclic ring containing 1 or 2 optionally substituted heteroatoms, or R1 is hydrogen or halogen or optionally substituted alkyloxy or alkyl, and R2 is thioalkyl; R3 is hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxy or alkyloxycarbonyl; X is O or S or -NH-, -CO-, methylene, ethylene, alkylidene or 1,1-cycloalkyl; and Y is O or S. The novel products of general formula (I) are farnesyl transferase inhibitors having remarkable antitumoral and antineoplastic properties.
    • 公开了通式(I)的新产品,其制备方法和含有所述产物的药物组合物。 在通式(I)中,R为通式 - (CH2)m-X1-(CH2)nZ的基团,其中X1为单键或O或S,n为0或1,n为0,1或 2,CH2基任选被羧基,烷氧基羰基,氨基甲酰基,烷基氨基甲酰基,二烷基氨基甲酰基,氨基,烷基氨基或二烷基氨基取代,Z是羧基,COOR4,其中R4是烷基或CON(R5)(R6),其中R5是氢 或烷基,R 6是氢或任选取代的烷基,或者R 5是氢或烷基,R 6是羟基,任选取代的烷氧基或氨基或PO(OR 7)2,其中R 7是氢或烷基; 或其中T为氢或任选取代的烷基的基团-NH-CO-T; 或者一个激进的(a); R 1和R 2是氢或卤素或任选取代的烷氧基或烷基,或者R 1和R 2在邻位形成含有1或2个任选取代的杂原子的杂环,或R 1是氢或卤素或任选取代的烷氧基或烷基,R 2是 硫代; R3是氢或卤素或烷基,烯基,烷氧基,烷硫基,羧基或烷氧基羰基; X是O或S或-NH-,-CO-,亚甲基,亚乙基,亚烷基或1,1-环烷基; 并且Y是O或S.通式(I)的新产物是具有显着抗肿瘤和抗肿瘤性质的法呢基转移酶抑制剂。
    • 88. 发明申请
    • NOVEL TAXOIDS, PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    • 新型紫杉醇,其制剂及含有其的药物组合物
    • WO1996013494A1
    • 1996-05-09
    • PCT/FR1995001393
    • 1995-10-23
    • RHONE-POULENC RORER S.A.BOUCHARD, HervéBOURZAT, Jean-DominiqueCOMMERÇON, AlainTERRIER, CorinneZUCCO, Martine
    • RHONE-POULENC RORER S.A.
    • C07D305/14
    • C07D305/14
    • Novel taxoids of general formulas (I) and (II), preparation thereof, and pharmaceutical compositions containing same. In general formula (I), Ra is hydrogen, hydroxy, alkoxy, acyloxy or alkoxyacetoxy and Rb is hydrogen, or Ra and Rb, taken together with the carbon atom to which they are attached, form a ketone function; Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally substituted benzoyl, thenoyl or furoyl radical or a radical R2-O-CO- where R2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical; R3 is an aromatic heterocyclic, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or naphthyl radical; R4 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, aryl or heterocyclyl radical; and R5 is an optionally substituted cycloalkenyl, alkyl, alkenyl, alkynyl or cycloalkyl radical. The novel products of general formula (I), wherein Z is a radical of general formula (II), have remarkable antitumoral and antineoplastic properties.
    • 通式(I)和(II)的新型紫杉烷类,其制备方法和含有它们的药物组合物。 在通式(I)中,R a是氢,羟基,烷氧基,酰氧基或烷氧基乙酰氧基,R b是氢,或者R a和R b与它们所连接的碳原子一起形成酮官能团; Z是氢原子或通式(II)的基团,其中R 1是任选取代的苯甲酰基,噻吩甲酰基或糠基或基团R 2 -O-CO-,其中R 2是烷基,烯基,炔基,环烷基,环烯基, 任选取代的苯基或杂环基; R3是芳族杂环,烷基,烯基,炔基,环烷基,苯基或萘基; R4是烷基,烯基,炔基,环烷基,环烯基,双环烷基,芳基或杂环基; 并且R 5是任选取代的环烯基,烷基,烯基,炔基或环烷基。 通式(I)的新产物,其中Z为通式(II)的基团,具有显着的抗肿瘤和抗肿瘤性质。